A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators
Rodriguez A, Nong Y, Sekaran N, Alagille D, Tamagnan G, Conn P. A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators. Molecular Pharmacology 2005, 68: 1793-1802. PMID: 16155210, DOI: 10.1124/mol.105.016139.Peer-Reviewed Original ResearchConceptsMetabotropic glutamate receptor subtype 5Subtype 5Allosteric siteG protein-coupled receptorsProtein-coupled receptorsMajor excitatory neurotransmitterCentral nervous systemMPEP siteAntagonist MPEPBinding of glutamateOnly partial inhibitionExcitatory neurotransmitterSubthalamic nucleusCalcium mobilizationNervous systemSite ligandsAllosteric modulatorsPartial antagonistValuable new toolNovel compoundsValuable new insightsOrthosteric ligandsAllosteric modulationFunctional effectsNative systems